Multitarget AD-IN-8
Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C31H34N2O8
- Molecular Weight:562.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
BACE1 |
Bax |
Bcl-2 |
Caspase-1 |
ERK1 |
ERK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PC-12 | EC50 |
1.24 μM
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Neuroprotective activity against Aβ25-35-induced injury in PC12 cells assessed as increase in cell viability incubated for 24 hrs by CCK-8 assay.
Neuroprotective activity against Aβ25-35-induced injury in PC12 cells assessed as increase in cell viability incubated for 24 hrs by CCK-8 assay.
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42628381 |
In Vitro
Multitarget AD-IN-8 (Compound S12) (20 μM) demonstrates potent neuroprotective activity against Aβ25-35 induced injury in PC12 cells with an EC50 of 1.24 μM[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) suppresses the aberrant phosphorylation of tau protein at Thr181 and Ser396 in PC12 cells[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) inhibits the Aβ25-35 induced activation of the NF-κB signaling pathway in PC12 cells[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) suppresses Aβ25-35 induced activation of the MAPK signaling pathway in PC12 cells[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) inhibits the production of BACE1 in PC12 cells induced by Aβ25-35[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) inhibits the activation of the Bax/Bcl-2 pathway and suppresses caspase-1 activation in PC12 cells[1].
Multitarget AD-IN-8 (20 μM; 24 h) effectively suppresses Aβ25-35 induced apoptosis in PC12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC12
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Concentration:5-20 μM
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Incubation Time:1 h (pretreatment); 24 h (Aβ25-35 exposure)
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Result:Markedly attenuated Aβ25-35 induced hyperphosphorylation of tau at Thr181 and Ser396 residues.
Inhibited the relative protein expression of p-Tau (Thr181)/Total-Tau and p-Tau (Ser396)/Total-Tau.\nAt a concentration of 20 μM, significantly attenuated Aβ25-35 induced phosphorylation of NF-κB.
Exhibited greater inhibitory activity than both donepezil and UA.\nAttenuated the Aβ25-35 induced upregulation of p-p38/p38, p-ERK1/2/ERK1/2, and p-JNK/JNK.\nMarkedly attenuated the Aβ25-35 induced BACE1 upregulation.\nAttenuated the Aβ25-35 induced upregulation of the Bax/Bcl-2 ratio and caspase-1 expression.
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Cell Line:PC12
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Concentration:20 μM
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Incubation Time:24 h
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Result:Reduced the percentage of apoptotic PC12 cells to 11%, compared to the Aβ25-35 group which had an apoptosis rate of 35.2%.
In Vivo
Multitarget AD-IN-8 (12.5-50 mg/kg; i.g.; daily; 20 consecutive days) exhibits no overt toxicity in major organs including the heart, liver, spleen, and kidneys in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (Male, 20-25 g)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:i.g.; daily; 21 consecutive days
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Result:Ameliorated the alternation behavior deficit in the Y-maze test.
Increased the discrimination index (DI) and preference index (PI) at 1 h and 24 h in the novel object recognition test.
Decreased escape latency and swimming distance in the Morris water maze, with the 50 mg/kg group differing significantly from the model group.
Increased time spent in and distance traveled within the target quadrant in the spatial probe test, with the 50 mg/kg group showing the most pronounced improvement.
Resulted in a more organized neuronal architecture and significantly attenuated neuronal damage in both the CA1 and CA3 regions.
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Animal Model:ICR mice (Male)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:i.g.; daily; 20 consecutive days
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Result:No abnormal behavior, mortality, or clinically significant changes in body weight were observed.
HE staining of major organs (heart, liver, spleen, and kidney) showed no obvious pathological lesions in all groups.
Chemical Information
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Molecular Weight 562.61
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Formula C31H34N2O8
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SMILES
CC(C1=C(O)C(C)=C(O)C([C@@]2(C)C(/C3=C(NC4=CC=C(OC(N(CCC)CCC)=O)C=C4)/C)=O)=C1OC2=CC3=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Protocol for Water Maze
The Morris Water Maze is a rodent spatial learning and memory assay in which a mouse or rat swims in opaque water to find an escape platform; in the hidden-platform version, the animal cannot see the platform and must use distal extra-maze cues to learn its fixed spatial location. The assay primarily measures hippocampus-dependent spatial learning during acquisition trials and spatial reference memory during probe trials after platform removal; readouts include escape latency, swim path length, swim speed, quadrant occupancy, platform-site crossings, and proximity to the former platform location.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Protocol for Shuttle Box Test (TDPA)
The Shuttle Box Test for TDPA, or temporally dissociated passive avoidance, measures hippocampus-dependent associative learning by testing whether a rodent avoids entering a dark compartment that was previously paired with foot shock after a temporal delay between dark-compartment entry and shock delivery. The main behavioral readout is crossover or step-through latency from the light chamber into the dark chamber; increased latency across training or retention trials reflects learned avoidance memory rather than motor performance alone.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)